New type of painkiller effective with mice for chronic pain, researchers say

Researchers found a new class of small-molecule compounds designed to treat pain linked to sunburns, may also work for conditions in the pancreas and colon.

By Stephen Feller

DURHAM, N.C., June 4 (UPI) -- Research into new types of painkillers to treat pain from sunburns and painful sensations originating in the head and face has led researchers to find a new class of drugs that may be effective for certain types of pain linked to pancreas and colon conditions.

Researchers at Duke University found a small-molecule compound designed to treat pain linked to the molecule TRPV4 in the skin also blocks a molecule called TRPA1, which is connected to pain from nerve conditions, the pancreas and possibly other aches originating in internal organs.


The TRP group of ion channels function in sensory nerve cells to sense painful stimuli, which researchers have been working to block to help alleviate pain in patients with chronic conditions.

Following the success of a molecule that successfully blocked TRPV4 in 2009, the researchers continuing working for stronger types of their successful prototype drug, stumbling onto the candidate drug used in the new study, called 16-8, which was 10 times more effective in cells in lab tests.

"As a physician, I soon realized the enormous potential that these compounds might have, given how beneficial dual-target molecules can be in clinical medicine," Dr. Wolfgana Liedtke, a professor of neurology, anesthesiology and neurobiology at the Duke University School of Medicine, said in a press release.


For the study, published in the journal Scientific Reports, the researchers tested a series of compounds' effects on cells in the lab, finding several to be effective but that one referred to as 16-8 had the greatest blocking effect on TRPV4.

They were surprised to also find it's efficacy against TRPA1, widening its efficacy against skin disorders to also include degenerative or inflammatory musculoskeletal conditions. In experiments with mice, the compound was effective against pancreatitis.

The researchers plan to explore the compounds' effects on other conditions as well, including creating topical applications for mucous membranes.

"We are very pleased with what is a first chapter in a highly promising story," Liedtke said. "We hope to be able to develop these compounds for clinical use in humans or animals."

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